Through its interaction with receptors borne on neuronal and other cells, 5-hydroxytryptamine (5-HT; serotonin), exerts various physiological effects. Imbalances in this interaction are believed to be responsible for such conditions as anxiety, depression, hallucination, migraine, chemotherapy-induced nausea, and for disorders in sexual activity, cardiovascular activity and thermoregulation, among others. From an improved understanding of the 5-HT receptor population, it is apparent that these effects are mediated selectively through individual types and sub-types of 5-HT receptors. Migraine, for example, has been treated with ergotamine, dihydroergotamine and methysergide, all of which act at 5-HT-1D type receptors.
Given the physiological and clinical significance of the 5-HT-1D receptor, it would be desirable to provide compounds capable of binding with high affinity to this receptor, for medical use for example to treat indications such as migraine and others for which administration of a 5-HT-1D ligand is indicated, and also for diagnostic use for example to identify these receptors and to screen for drug candidates.